GlpBio

SRPIN340

目录号: GC13596纯度: >99.50%同义词: SRPK inhibitor
A selective inhibitor of SRPK1
SRPIN340
Cas No.: 218156-96-8
规格价格库存数量操作
5mg¥483.00现货
1
10mg¥746.00现货
1
25mg¥1,659.00现货
1
50mg¥2,541.00现货
1
100mg¥5,880.00现货
1
10mM (in 1mL DMSO)¥525.00现货
1
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文献被引

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产品描述 Description

SRPIN340 is a highly selective inhibitor of SR protein phosphorylation with a Ki value of 0.89μM for SRPK1 [1].

SRPIN340 has been revealed to inhibit replication of HIV-1 and other viruses that require SR protein-dependent RNA processing for the propagation in HIV-1 transfected or infected Flp-In293 cell lines. In addition, SRPIN340 has been reported to significantly inhibit SRPK1 and SRPK2 kinase activity but not potently inhibit other SRPKs, such as Clk1 and Clk4 with a Ki value of 0.89μM for SRPK1. Besides, SRPIN340 has been exhibited to dose-dependently promote degradation of SRp75 which is necessary for HIV expression. Moreover, SRPIN340 has shown the inhibition of propagation of Sindbis virus with an IC50 of 60μM and the protection against the cytopathic effect of Sindbis virus [1].

References:
[1] Fukuhara T1, Hosoya T, Shimizu S, Sumi K, Oshiro T, Yoshinaka Y, Suzuki M, Yamamoto N, Herzenberg LA, Herzenberg LA, Hagiwara M.Utilization of host SR protein kinases and RNA-splicing machinery during viral replication. Proc Natl Acad Sci U S A. 2006 Jul 25;103(30):11329-33. Epub 2006 Jul 13.

实验参考方法 Experimental Reference Method

Cell experiment [1]:

Cell lines

A375, Omm2.5, Mel270 and 92.1 cells

Preparation method

The solubility of this compound in DMSO is >10.9mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

10 μM; 24 hours

Applications

In A375 cells, SRPIN340 resulted in a 54% reduction in the IGF-1 induced nuclear localisation of SRSF1. In Mel270 cells, SRPIN340 significantly reduced the proportion of nuclear SRSF1 compared with IGF-1 treatment alone. In A375, Omm2.5 and 92.1 cells, SRPIN340 reduced total VEGF protein.
Animal experiment [1]:

Animal models

Mice bearing A375-untransfected tumours

Dosage form

100 μl of 20 μg/ml SRPIN340 (diluted 100× in PBS from 2mg/ml stock in DMSO); injected daily into the peritumoral space

Application

In mice bearing A375-untransfected tumours, SRPIN340 significantly reduced tumour growth compared with DMSO control-injected tumours. SRPIN340 also reduced total VEGF expression and significantly reduced microvascular density (MVD).

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. M V Gammons, R Lucas, R Dean, et al. Targeting SRPK1 to control VEGF-mediated tumour angiogenesis in metastatic melanoma. Br J Cancer. 2014 Jul 29; 111(3): 477-485.

产品文档 Product Documents

Purity:>99.50%

化学性质Chemical Properties

CAS 号
218156-96-8
同义词
SRPK inhibitor
化学名
N-[2-piperidin-1-yl-5-(trifluoromethyl)phenyl]pyridine-4-carboxamide
SMILES
C1CCN(CC1)C2=C(C=C(C=C2)C(F)(F)F)NC(=O)C3=CC=NC=C3
分子式
C18H18F3N3O
分子量
349.35 g/mol
溶解性
≥ 10.9mg/mL in DMSO
保存条件
Store at -20°C
General tips
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备 RT，或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol